General Information of Drug (ID: DM1FDN8)

Drug Name
Mizolastine Drug Info
Synonyms
Mistalin; Mistamine; Mizolastina; Mizolastinum; Mizolen; Mizollen; Zolim; Zolistam; Zolistan; Allphar brand of mizolastine; Galderma brand of mizolastine; Mizolastine [INN]; Novag brand of mizolastine; Sanofi Synthelabo brand of mizolastine; Schwarz brand of mizolastine; MKC-431; Mizolastina [INN-Spanish]; Mizolastinum [INN-Latin]; Mizollen (TN); SL 85.0324; Mizolastine (JAN/INN); SL-85.0324; 2-((1-(1-(p-Fluorobenzyl)-2-benzimidazolyl)-4-piperidyl)methylamino)-4(3H)-pyrimidinone; 2-[[1-[1-[(4-fluorophenyl)methyl]benzimidazol-2-yl]piperidin-4-yl]-methylamino]-1H-pyrimidin-6-one
Indication
Disease Entry ICD 11 Status REF
Allergic rhinitis CA08.0 Approved [1]
Therapeutic Class
Antiallergic Agents
Cross-matching ID
PubChem CID
65906
ChEBI ID
CHEBI:31857
CAS Number
CAS 108612-45-9
TTD Drug ID
DM1FDN8
VARIDT Drug ID
DR00777

Molecule-Related Drug Atlas

Molecule-Related Drug Atlas
Molecule Type:
DTT
DOT
Drug Status:
Approved Drug(s)
Drug(s) Targeting Histamine H1 receptor (H1R)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Ergotidine DM78IME Osteoarthritis FA00-FA05 Approved [5]
Loratadine DMF3AN7 Allergy 4A80-4A85 Approved [6]
Azelastine DMXTMBJ Allergic conjunctivitis 9A60.02 Approved [7]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [8]
Cinnarizine DM7U5QJ Meniere disease AB31.0 Approved [9]
Diphenhydramine DMKQTBA Hyperemesis gravidarum Approved [7]
Doxepin DMPI98T Anxiety Approved [10]
Chlorpheniramine DM5URA2 Allergic rhinitis CA08.0 Approved [7]
Epinastine DMX0K3Q Allergic conjunctivitis 9A60.02 Approved [11]
Desloratadine DM56YN7 Allergic rhinitis CA08.0 Approved [12]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [13]
Dicloxacillin DM8EU0Z Bacterial infection 1A00-1C4Z Approved [13]
Ergonovine DM0VEC1 Postpartum haemorrhage JA43 Approved [14]
Cannabidiol DM0659E Dravet syndrome 8A61.11 Approved [15]
Fexofenadine DM17ONX Allergic rhinitis CA08.0 Approved [16]
Hydrogen peroxide DM1NG5W Infectious disease 1A00-CA43.1 Approved [17]
Ribavirin DMEYLH9 Hepatitis C virus infection 1E51.1 Approved [18]
Salicyclic acid DM2F8XZ Acne vulgaris ED80 Approved [19]
TECFIDERA DM2OVDT Multiple sclerosis 8A40 Approved [20]
Sulindac DM2QHZU Acute myelogenous leukaemia 2A41 Approved [21]
⏷ Show the Full List of 10 Drug(s)
Drug Name Drug ID Indication ICD 11 Highest Status REF
Metoclopramide DMFA5MY Nausea MD90 Approved [22]
Quinidine DMLPICK N. A. N. A. Approved [23]
Verapamil DMA7PEW Angina pectoris BA40 Approved [24]
Erythromycin DM4K7GQ Acne vulgaris ED80 Approved [25]
Clarithromycin DM4M1SG Acute maxillary sinusitis Approved [25]
Disopyramide DM5SYZP Long QT syndrome BC65.0 Approved [26]
Propranolol DM79NTF Angina pectoris BA40 Approved [27]
Amiodarone DMUTEX3 Tachyarrhythmias BC71 Approved [28]
Dofetilide DMPN1TW Sinus rhythm disorder BC9Y Approved [29]
Flecainide DMSQDLE Tachyarrhythmias BC71 Approved [25]
⏷ Show the Full List of 10 Drug(s)

Molecular Interaction Atlas of This Drug

Molecular Interaction Atlas

Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Histamine H1 receptor (H1R) TTTIBOJ HRH1_HUMAN Antagonist [2]

Drug Off-Target (DOT)
DOT Name DOT ID UniProt ID Interaction REF
Intercellular adhesion molecule 1 (ICAM1) OTTOIX77 ICAM1_HUMAN Gene/Protein Processing [3]
Potassium voltage-gated channel subfamily H member 2 (KCNH2) OTZX881H KCNH2_HUMAN Gene/Protein Processing [4]

References

1 Population pharmacokinetic analysis and optimization of the experimental design for mizolastine solution in children. J Pharmacokinet Pharmacodyn. 2001 Jun;28(3):299-319.
2 Histamine H1-receptor antagonists inhibit nuclear factor-kappaB and activator protein-1 activities via H1-receptor-dependent and -independent mechanisms. Clin Exp Allergy. 2008 Jun;38(6):947-56.
3 Antiallergic effects of H1-receptor antagonists. Allergy. 2000;55 Suppl 64:17-27. doi: 10.1034/j.1398-9995.2000.00803.x.
4 Inhibition of HERG1 K(+) channels by the novel second-generation antihistamine mizolastine. Br J Pharmacol. 2000 Nov;131(6):1081-8. doi: 10.1038/sj.bjp.0703654.
5 Cloning and pharmacological characterization of a fourth histamine receptor (H(4)) expressed in bone marrow. Mol Pharmacol. 2001 Mar;59(3):420-6.
6 Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis. Lin Chung Er Bi Yan Hou Tou Jing Wai Ke Za Zhi. 2009 Jan;23(2):63-6.
7 Intact cell binding for in vitro prediction of sedative and non-sedative histamine H1-receptor antagonists based on receptor internalization. J Pharmacol Sci. 2008 May;107(1):66-79.
8 Update on prescription and over-the-counter histamine inverse agonists in rhinitis therapy. Curr Allergy Asthma Rep. 2009 Mar;9(2):140-8.
9 Central effects of cinnarizine: restricted use in aircrew. Aviat Space Environ Med. 2002 Jun;73(6):570-4.
10 Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
11 Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
12 Examining the tolerability of the non-sedating antihistamine desloratadine: a prescription-event monitoring study in England. Drug Saf. 2009;32(2):169-79.
13 Dicloxacillin and erythromycin at high concentrations increase ICAM-1 expression by endothelial cells: a possible factor in the pathogenesis of infusion phlebitis. J Antimicrob Chemother. 2004 Feb;53(2):174-9. doi: 10.1093/jac/dkh056. Epub 2004 Jan 16.
14 ADReCS-Target: target profiles for aiding drug safety research and application. Nucleic Acids Res. 2018 Jan 4;46(D1):D911-D917. doi: 10.1093/nar/gkx899.
15 Cannabidiol inhibits lung cancer cell invasion and metastasis via intercellular adhesion molecule-1. FASEB J. 2012 Apr;26(4):1535-48. doi: 10.1096/fj.11-198184. Epub 2011 Dec 23.
16 The effect of fexofenadine on expression of intercellular adhesion molecule 1 and induction of apoptosis on peripheral eosinophils. Allergy Asthma Proc. 2005 Jul-Aug;26(4):292-8.
17 Cytokine mRNA profiles in cultured human skin component cells exposed to various chemicals: a simulation model of epicutaneous stimuli induced by skin barrier perturbation in comparison with that due to exposure to haptens or irritant. J Dermatol Sci. 2001 Jun;26(2):85-93. doi: 10.1016/s0923-1811(00)00165-1.
18 Correlation of sICAM-1 and sVCAM-1 level with biochemical, histological and viral findings in chronic hepatitis C after interferon-alpha + ribavirin therapy. Rom J Gastroenterol. 2003 Jun;12(2):91-5.
19 Some non-sensitizers upregulate CD54 expression by activation of the NLRP3 inflammasome in THP-1 cells. J Toxicol Sci. 2019;44(3):213-224. doi: 10.2131/jts.44.213.
20 Dimethyl Fumarate Inhibits the Nuclear Factor B Pathway in Breast Cancer Cells by Covalent Modification of p65 Protein. J Biol Chem. 2016 Feb 12;291(7):3639-47. doi: 10.1074/jbc.M115.679704. Epub 2015 Dec 18.
21 The proapoptotic effects of sulindac, sulindac sulfone and indomethacin are mediated by nucleolar translocation of the RelA(p65) subunit of NF-kappaB. Oncogene. 2008 Apr 17;27(18):2648-55. doi: 10.1038/sj.onc.1210891. Epub 2007 Dec 3.
22 Comparison of the effects of metoclopramide and domperidone on HERG channels. Pharmacology. 2005 Apr;74(1):31-6. doi: 10.1159/000083234. Epub 2005 Jan 7.
23 Further insights into the effect of quinidine in short QT syndrome caused by a mutation in HERG. J Cardiovasc Electrophysiol. 2005 Jan;16(1):54-8. doi: 10.1046/j.1540-8167.2005.04470.x.
24 Automated tight seal electrophysiology for assessing the potential hERG liability of pharmaceutical compounds. Assay Drug Dev Technol. 2004 Oct;2(5):497-506. doi: 10.1089/adt.2004.2.497.
25 Refining the human iPSC-cardiomyocyte arrhythmic risk assessment model. Toxicol Sci. 2013 Dec;136(2):581-94. doi: 10.1093/toxsci/kft205. Epub 2013 Sep 19.
26 Pharmacology of the short QT syndrome N588K-hERG K+ channel mutation: differential impact on selected class I and class III antiarrhythmic drugs. Br J Pharmacol. 2008 Nov;155(6):957-66. doi: 10.1038/bjp.2008.325. Epub 2008 Aug 25.
27 Comparison of HERG channel blocking effects of various beta-blockers-- implication for clinical strategy. Br J Pharmacol. 2006 Mar;147(6):642-52. doi: 10.1038/sj.bjp.0706508.
28 Inhibitory effects of the class III antiarrhythmic drug amiodarone on cloned HERG potassium channels. Naunyn Schmiedebergs Arch Pharmacol. 1999 Mar;359(3):212-9. doi: 10.1007/pl00005344.
29 Redox state dependency of HERGS631C channel pharmacology: relation to C-type inactivation. FEBS Lett. 2000 May 26;474(1):111-5. doi: 10.1016/s0014-5793(00)01586-6.